KR20230095923A - Jak1 억제제를 제조하기 위한 공정 및 중간체 - Google Patents

Jak1 억제제를 제조하기 위한 공정 및 중간체 Download PDF

Info

Publication number
KR20230095923A
KR20230095923A KR1020237009250A KR20237009250A KR20230095923A KR 20230095923 A KR20230095923 A KR 20230095923A KR 1020237009250 A KR1020237009250 A KR 1020237009250A KR 20237009250 A KR20237009250 A KR 20237009250A KR 20230095923 A KR20230095923 A KR 20230095923A
Authority
KR
South Korea
Prior art keywords
formula
compound
salt
reacting
prepared
Prior art date
Application number
KR1020237009250A
Other languages
English (en)
Korean (ko)
Inventor
자청 저우
스리 천
핑리 류
데이비드 제이. 멜로니
융춘 판
나이징 수
마이클 샤
Original Assignee
인사이트 코포레이션
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by 인사이트 코포레이션 filed Critical 인사이트 코포레이션
Publication of KR20230095923A publication Critical patent/KR20230095923A/ko

Links

Images

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D205/00Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/04Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/55Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Health & Medical Sciences (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
KR1020237009250A 2020-08-18 2021-08-17 Jak1 억제제를 제조하기 위한 공정 및 중간체 KR20230095923A (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US202063067062P 2020-08-18 2020-08-18
US63/067,062 2020-08-18
PCT/US2021/046286 WO2022040172A1 (en) 2020-08-18 2021-08-17 Process and intermediates for preparing a jak1 inhibitor

Publications (1)

Publication Number Publication Date
KR20230095923A true KR20230095923A (ko) 2023-06-29

Family

ID=77693614

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020237009250A KR20230095923A (ko) 2020-08-18 2021-08-17 Jak1 억제제를 제조하기 위한 공정 및 중간체

Country Status (18)

Country Link
US (1) US11897889B2 (ja)
EP (1) EP4200278A1 (ja)
JP (1) JP2023538614A (ja)
KR (1) KR20230095923A (ja)
CN (1) CN117043152A (ja)
AR (1) AR123268A1 (ja)
AU (1) AU2021329301A1 (ja)
BR (1) BR112023002939A2 (ja)
CA (1) CA3192055A1 (ja)
CL (1) CL2023000482A1 (ja)
CO (1) CO2023003286A2 (ja)
CR (1) CR20230130A (ja)
EC (1) ECSP23019419A (ja)
IL (1) IL300557A (ja)
MX (1) MX2023002035A (ja)
PE (1) PE20231308A1 (ja)
TW (1) TW202212341A (ja)
WO (1) WO2022040172A1 (ja)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA3192055A1 (en) 2020-08-18 2022-02-24 Incyte Corporation Process and intermediates for preparing a jak1 inhibitor
US11905292B2 (en) 2020-08-18 2024-02-20 Incyte Corporation Process and intermediates for preparing a JAK inhibitor
WO2023288197A1 (en) * 2021-07-12 2023-01-19 Incyte Corporation Process and intermediates for preparing baricitinib

Family Cites Families (65)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB812366A (en) 1955-08-18 1959-04-22 Wellcome Found Improvements in and relating to derivatives of pyrimidine and the preparation thereof
US5102904A (en) 1989-12-08 1992-04-07 American Cyanamid Company N-oxygenated arylpyrrole insecticidal, acaricidal and nematicidal agents and use thereas
US20050288503A1 (en) 2002-09-06 2005-12-29 Adams Jerry L Novel compounds
EP1773836B1 (en) 2004-05-27 2012-09-05 Pfizer Products Inc. Pyrrolopyrimidine derivatives useful in cancer treatment
AR054416A1 (es) 2004-12-22 2007-06-27 Incyte Corp Pirrolo [2,3-b]piridin-4-il-aminas y pirrolo [2,3-b]pirimidin-4-il-aminas como inhibidores de las quinasas janus. composiciones farmaceuticas.
AU2006273762A1 (en) 2005-07-29 2007-02-01 Pfizer Products Inc. Pyrrolo[2,3-d]pyrimidine derivatives; their intermediates and synthesis
SI3184526T1 (sl) 2005-12-13 2019-03-29 Incyte Holdings Corporation Derivati pirolo(2,3-D)pirimidina kot inhibitorji Janus kinaze
CN2928286Y (zh) 2006-01-06 2007-08-01 水城钢铁(集团)有限责任公司 预入口导卫装置
KR101450535B1 (ko) 2006-02-02 2014-10-14 밀레니엄 파머슈티컬스 인코퍼레이티드 E1 활성화 효소의 억제제
PL2173752T5 (pl) 2007-06-13 2022-12-05 Incyte Holdings Corporation Sole (r)-3-(4-(7h-pirolo(2,3-d)pirymidyn-4-ylo)-1h-pirazol-1-ilo)-3-cyklopentylopropanonitrylu inhibitora kinazy janusowej
CL2008001709A1 (es) 2007-06-13 2008-11-03 Incyte Corp Compuestos derivados de pirrolo [2,3-b]pirimidina, moduladores de quinasas jak; composicion farmaceutica; y uso en el tratamiento de enfermedades tales como cancer, psoriasis, artritis reumatoide, entre otras.
CA2695114A1 (en) 2007-08-01 2009-02-05 Pfizer Inc. Pyrazole compounds and their use as raf inhibitors
UA104849C2 (uk) 2007-11-16 2014-03-25 Інсайт Корпорейшн 4-піразоліл-n-арилпіримідин-2-аміни і 4-піразоліл-n-гетероарилпіримідин-2-аміни як інгібітори кіназ janus
EA017218B1 (ru) 2008-03-11 2012-10-30 Инсайт Корпорейшн Производные азетидина и циклобутана как ингибиторы jak-киназ
CL2009001884A1 (es) 2008-10-02 2010-05-14 Incyte Holdings Corp Uso de 3-ciclopentil-3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)propanonitrilo, inhibidor de janus quinasa, y uso de una composición que lo comprende para el tratamiento del ojo seco.
JOP20190230A1 (ar) 2009-01-15 2017-06-16 Incyte Corp طرق لاصلاح مثبطات انزيم jak و المركبات الوسيطة المتعلقة به
JP2012523405A (ja) 2009-04-10 2012-10-04 ファイザー・インク 4,5−ジヒドロ−1h−ピラゾール化合物およびその薬学的使用
MX2011012262A (es) 2009-05-22 2012-01-25 Incyte Corp 3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il] octano-o heptano-nitrilo como inhibidores de cinasas janus (jak).
EP2432555B1 (en) 2009-05-22 2014-04-30 Incyte Corporation N-(hetero)aryl-pyrrolidine derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines and pyrrol-3-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
AR078012A1 (es) 2009-09-01 2011-10-05 Incyte Corp Derivados heterociclicos de las pirazol-4-il- pirrolo (2,3-d) pirimidinas como inhibidores de la quinasa janus
EP2486041B1 (en) 2009-10-09 2013-08-14 Incyte Corporation Hydroxyl, keto, and glucuronide derivatives of 3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile
KR20120102669A (ko) 2009-11-06 2012-09-18 플렉시콘, 인코퍼레이티드 키나제 조정을 위한 화합물 및 방법, 및 이를 위한 적응증
US8673928B2 (en) 2009-11-18 2014-03-18 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
US20110207754A1 (en) 2010-02-18 2011-08-25 Incyte Corporation Cyclobutane and methylcyclobutane derivatives as janus kinase inhibitors
SI3354652T1 (sl) 2010-03-10 2020-08-31 Incyte Holdings Corporation Derivati piperidin-4-il azetidina kot inhibitorji JAK1
TWI510487B (zh) 2010-04-21 2015-12-01 Plexxikon Inc 用於激酶調節的化合物和方法及其適應症
DK2574168T3 (en) 2010-05-21 2016-05-09 Incyte Holdings Corp Topical formulation to a jak inhibitor
ES2536415T3 (es) 2010-11-19 2015-05-25 Incyte Corporation Pirrolopiridinas y pirrolopirimidinas sustituidas heterocíclicas como inhibidores de JAK
PE20140146A1 (es) 2010-11-19 2014-02-06 Incyte Corp Derivados de pirrolopiridina y pirrolopirimidina sustituidos con ciclobutilo como inhibidores de jak
MY165963A (en) 2011-06-20 2018-05-18 Incyte Holdings Corp Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors
CN103732597B (zh) * 2011-08-12 2016-08-17 日产化学工业株式会社 三环杂环化合物和jak抑制剂
TW201313721A (zh) 2011-08-18 2013-04-01 Incyte Corp 作為jak抑制劑之環己基氮雜環丁烷衍生物
UA111854C2 (uk) 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки для отримання інгібіторів jak
WO2013173720A1 (en) 2012-05-18 2013-11-21 Incyte Corporation Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors
MY191357A (en) 2012-11-15 2022-06-19 Incyte Holdings Corp Sustained-release dosage forms of ruxolitinib
MX2015011667A (es) 2013-03-06 2015-12-16 Incyte Corp Procesos e intermedios para hacer un inhibidor de jak.
TWI664176B (zh) 2013-05-17 2019-07-01 英塞特公司 作為jak抑制劑之聯吡唑衍生物
SG10201912203XA (en) 2013-08-07 2020-02-27 Incyte Corp Sustained release dosage forms for a jak1 inhibitor
EP3137471A1 (en) 2014-04-30 2017-03-08 Incyte Corporation Processes of preparing a jak1 inhibitor and new forms thereto
WO2016026975A1 (en) 2014-08-21 2016-02-25 Ratiopharm Gmbh Salt of (r)-3-(4-(7h-pyrrolo [2,3-d] pyrimidin-4-yl)-lh-pyrazol-l-yl)-3-cyclopentylpropanenitrile with benzenesulfonic acid
EP3183252B1 (en) 2014-08-21 2021-05-12 ratiopharm GmbH Oxalate salt of ruxolitinib
WO2016035014A1 (en) 2014-09-01 2016-03-10 Sun Pharmaceutical Industries Limited Processes for the preparation of ruxolitinib phosphate
WO2016063294A2 (en) 2014-10-20 2016-04-28 Msn Laboratories Private Limited Process for the preparation of (r)-3-(4-(7h-pyrrolo[2,3-d], pyrimidin-4-yl)-1 h-pyrazol-1-yl)-3-cyclopentylpropanenitrile phosphate and its polymorphs thereof
AU2016225133B2 (en) 2015-02-24 2018-11-29 Pfizer Inc. Substituted nucleoside derivatives useful as anticancer agents
CN106397443A (zh) 2015-07-17 2017-02-15 浙江九洲药业股份有限公司 一种吡咯嘧啶类衍生物中间体的制备方法
CZ2015575A3 (cs) 2015-08-26 2017-03-08 Zentiva, K.S. Soli 5-fluoro-3-fenyl-2-[(1S)-1-(9H-purin-6-ylamino)propyl]quinazolin-4-onu a jejich příprava
AU2016379454B2 (en) 2015-12-23 2021-01-28 The University Of British Columbia Lipid-linked prodrugs
WO2017114461A1 (zh) 2015-12-31 2017-07-06 正大天晴药业集团股份有限公司 一种芦可替尼的合成工艺
CZ201629A3 (cs) 2016-01-22 2017-08-02 Zentiva, K.S. Krystalické modifikace solí (3R)-3-cyklopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]propannitrilu a způsoby jejich přípravy
CN107513069A (zh) 2016-06-16 2017-12-26 正大天晴药业集团股份有限公司 手性吡咯并嘧啶化合物的制备方法
IN201641026603A (ja) 2016-08-04 2018-02-09
CN107722012B (zh) 2016-08-11 2020-05-29 斯福瑞(南通)制药有限公司 制备4-氯-7H-吡咯并[2,3-d]嘧啶的方法
CN107759601B (zh) 2016-08-23 2020-09-11 苏州旺山旺水生物医药有限公司 一种jak抑制剂及其盐的制备方法
CN107759623B (zh) 2016-08-23 2020-08-14 苏州旺山旺水生物医药有限公司 Jak抑制剂的中间体及其制备方法
EP3515909A1 (en) 2016-09-23 2019-07-31 Cellipse Lim kinase inhibitors, pharmaceutical composition and method of use in limk-mediated diseases
CN109651424B (zh) 2017-10-11 2021-01-22 新发药业有限公司 一种7-保护基-4-(1-氢-吡唑-4-基)吡咯[2,3-d]嘧啶的合成方法
US10766900B2 (en) 2017-12-29 2020-09-08 Formosa Laboratories, Inc. Baricitinib intermediate, method for forming Baricitinib intermediate, and method for preparing Baricitinib or pharmaceutically acceptable salt thereof
CN112105608B (zh) 2018-01-30 2023-07-14 因赛特公司 制备(1-(3-氟-2-(三氟甲基)异烟碱基)哌啶-4-酮)的方法
FI3797099T3 (fi) 2018-05-21 2024-01-30 Pi Industries Ltd Menetelmä substituoitujen heterosyklisten yhdisteiden valmistamiseksi
AU2020219797A1 (en) 2019-02-06 2021-09-02 Sun Pharmaceutical Industries, Inc. Process for preparing enantiomerically enriched jak inhibitors
CN110724145A (zh) 2019-11-01 2020-01-24 廖文杰 一种医药中间体4-氯吡咯并嘧啶的合成方法
CA3192055A1 (en) 2020-08-18 2022-02-24 Incyte Corporation Process and intermediates for preparing a jak1 inhibitor
US11905292B2 (en) 2020-08-18 2024-02-20 Incyte Corporation Process and intermediates for preparing a JAK inhibitor
WO2023288197A1 (en) 2021-07-12 2023-01-19 Incyte Corporation Process and intermediates for preparing baricitinib
CN113480546A (zh) 2021-07-30 2021-10-08 江苏君若药业有限公司 巴瑞克替尼及其衍生物的制备

Also Published As

Publication number Publication date
CR20230130A (es) 2023-07-13
IL300557A (en) 2023-04-01
WO2022040172A1 (en) 2022-02-24
US20220056034A1 (en) 2022-02-24
TW202212341A (zh) 2022-04-01
CL2023000482A1 (es) 2023-09-29
AU2021329301A1 (en) 2023-04-13
AR123268A1 (es) 2022-11-16
CA3192055A1 (en) 2022-02-24
CN117043152A (zh) 2023-11-10
US11897889B2 (en) 2024-02-13
MX2023002035A (es) 2023-06-12
ECSP23019419A (es) 2023-04-28
PE20231308A1 (es) 2023-08-24
CO2023003286A2 (es) 2023-06-09
EP4200278A1 (en) 2023-06-28
JP2023538614A (ja) 2023-09-08
BR112023002939A2 (pt) 2023-04-25

Similar Documents

Publication Publication Date Title
JP6640297B2 (ja) Jak阻害剤の製造方法及びその中間体
KR20230095923A (ko) Jak1 억제제를 제조하기 위한 공정 및 중간체
JP2022520047A (ja) 鏡像異性的に濃縮されたjak阻害剤を調製するための方法
KR20200129099A (ko) (1-(3-플루오로-2-(트리플루오로메틸)이소니코티닐)피페리딘-4-온)의 제조 방법
US20230059389A1 (en) Process and intermediates for preparing a jak inhibitor
JP2018535260A (ja) キナーゼ阻害剤およびその中間体の調製方法
JP2022504620A (ja) 甲状腺ホルモン受容体ベータアゴニスト化合物
US20240166655A1 (en) Process and intermediates for preparing a jak inhibitor
JP2006527769A (ja) Cb1モジュレーターとしての2,3位置換5,6−ジアリール−ピラジン誘導体
CN115989226A (zh) 制备jak抑制剂的方法和中间体
JP5711669B2 (ja) スピロケタール誘導体の製造方法
CN116761792A (zh) 用于制备jak抑制剂的方法和中间体
CN106604917B (zh) 作为醛固酮合酶抑制剂的新型二氢喹啉吡唑基化合物
CN117677616A (zh) 制备血红蛋白调节剂的方法